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[摘要]：Peripheral benzodiazepine receptor (PBR) is associated with neuroinflammation and tumor progression. [C-11]DAA1106 and [F-18]FEDAA1106 are two promising radioligands for positron emission tomography (PET) imaging of PBR. This study was designed to develop a new radiolabeled analog of [C-11]DAA1106 and [F-18]FEDAA1106, [C-11]FEDAA1106, for PET imaging of PBR expression in brain and cancer. Precursor N-(5-fluoro-2-phenoxyphenyl)-N-(2-(2-fluoroethoxy)-5-hydroxybenzyl)acetamide (9) was synthesized in multiple steps with moderate to high chemical yields. Precursor 9 was labeled by [C-11]CH3OTf and isolated by high pressure liquid chromatography (HPLC) purification to provide target radioligand N-(5-fluoro-2-phenoxyphenyl)-N-(2-(2-fluoroethoxy)-5-[C-11]methoxybenzyl)acetamide ([C-11]FEDAA1106, [C-11]10) in 60-70% radiochemical yields, decay corrected to end of bombardment (EOB), based on [C-11]CO2. The specific activity of the target radiotracer [C-11]10 was in a range of 111-185 GBq/mu mol at the end of synthesis (EOS). (C) 2008 Elsevier Masson SAS. All rights reserved. |
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